Ali Kazi Asraf, Chakraborty Rideb, Roy Sanjit Kr, Ghosal Kajal
Department of Pharmaceutical Technology, Maulana Abul Kalam Azad University of Technology, West Bengal, Nadia, PIN-741249, India.
Bengal College of Pharmaceutical Sciences and Research, Bidhannagar, Durgapur, West Bengal 713212, India.
Int J Biol Macromol. 2025 May;305(Pt 1):141105. doi: 10.1016/j.ijbiomac.2025.141105. Epub 2025 Feb 14.
Extended gastric residence of drugs can enhance the therapeutic effect, increase bioavailability, improve efficacy, and reduce the number of required doses by prolonging the retention of the drug delivery system. A new floating drug delivery for Ondansetron was designed and evaluated. Pre-formulation studies included the assessment of powder flow properties and drug-excipient compatibility. In-vitro release studies and a buoyancy test were performed to characterize the performance of the system. The study evaluated the properties of Ondansetron tablets. The optimized batches had compressibility index values ranging from 7.272 % to 25 %, with percentage weight fluctuation ranging from 0 to 1.05 %. The tablets were 2.92 and 3.52 mm thick, hardness between 3.50 and 4.65 kg/cm, and loss percentages between 0.12 and 0.68 %, except batch T8, which had high friability index values of 1.02. Thermo-gravimetric analysis and Differential scanning Calorimetry showed no interaction between the drug and other polymers. Formulations showed a sustained release of the drug for periods of >12 h for several compositions, while some showed a release of >90 %. The formulations with HPMC K4M showed slower drug release due to a strong hydro layer. Citric acid content increased drug release, suggesting modulation of drug release kinetics. Kinetic modeling revealed that some of the formulations exhibited zero-order release kinetics, which means that the drug is released at a constant rate to maintain a steady level of the drug in the body. This project aims to improve the therapeutic effect of Class I Biopharmaceutical Classification System (BCS I) drug ondansetron by using a stomach-retaining, floating drug delivery system. Promising results are indicative of better bioavailability and sustained therapeutic doses. Findings may influence the development of delivery methods for similar substances facing gastrointestinal absorption challenges.
药物在胃内的延长停留时间可增强治疗效果、提高生物利用度、改善疗效，并通过延长给药系统的滞留时间减少所需给药剂量。设计并评估了一种新型的昂丹司琼漂浮给药系统。处方前研究包括对粉体流动性和药物-辅料相容性的评估。进行了体外释放研究和浮力测试以表征该系统的性能。该研究评估了昂丹司琼片剂的性质。优化批次的压缩指数值在7.272%至25%之间，重量波动百分比在0至1.05%之间。片剂厚度为2.92和3.52毫米，硬度在3.50至4.65千克/平方厘米之间，除批次T8脆碎度指数值较高为1.02外，损失率在0.12%至0.68%之间。热重分析和差示扫描量热法表明药物与其他聚合物之间无相互作用。几种组合物的制剂显示药物持续释放>12小时，而有些则显示释放>90%。含羟丙甲纤维素K4M的制剂由于强水化层导致药物释放较慢。柠檬酸含量增加了药物释放，表明对药物释放动力学有调节作用。动力学建模表明，一些制剂呈现零级释放动力学，这意味着药物以恒定速率释放以维持体内药物的稳定水平。该项目旨在通过使用胃滞留漂浮给药系统提高I类生物药剂学分类系统（BCS I）药物昂丹司琼的治疗效果。有前景的结果表明生物利用度更高且治疗剂量持续。研究结果可能会影响面临胃肠道吸收挑战的类似物质给药方法的开发。
